BI-847325

SKU: orb1226796

Description

A novel ATP-competitive MEK/Aurora kinase inhibitor; inhibts human Aurora A (IC50=25 nM) and Aurora C(IC50=16 nM); also inhibits MEK1 (IC50=25 nM) and MEK2 (IC50=6 nM); reduces expression of p-ERK and p-Histone 3 in multiple models of vemurafenib resistance; decreases the expression of MEK and Mcl-1 and increases the expression of BIM; orally bioavailable.Solid Tumors Phase 1 Clinical(In Vitro):BI 847325 inhibits the activity of X. laevis AK-B with an IC50 of 3 nM; the IC50 values for human AK-A and AK-C are 25 and 15 nM, respectively. BI 847325 also inhibits human MEK1 and MEK2 with respective IC50 values of 25 and 4 nM. BI 847325 at 1,000 nM inhibits 6 enzymes by more than 50% (LCK, MAP3K8, FGFR1, AMPK, CAMK1D and TBK1) and the IC50 values are below 100 nM only for LCK (5 nM) and MAP3K8 (93 nM). Proliferation is inhibited in A375 and Calu-6 cell lines with GI50 values of 7.5 nM and 60 nM, respectively.(In Vivo):Daily oral administration of BI 847325 at 10 mg/kg shows efficacy in both BRAF- and KRAS-mutant xenograft models. BI 847325 administered once weekly at 70 mg/kg inhibits both MEK and AK in KRAS-mutant tumors.

Key Properties

• CAS Number: 1207293-36-4
• MW: 464.5582
• Purity: >98% (HPLC)
• Formula: C₂₉H₂₈N₄O₂
• SMILES: O=C(NCC)C#CC1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(CN(C)C)C=C3)/C4=CC=CC=C4
• Target: MEK
• Solubility: DMSO: ≥36 mg/mL

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BI847325 | BI 847325

Quick Database Links

Gene Symbol

MEK